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Opioid MoA = ? * Produces analgesia through actions at G protein-coupled receptors in the CNS and spinal cord
Opioids can be ? * Full agonists, partial agonists, or antagonists
Opioids have actions at ? * µ (mu) -, κ (kappa)-, or δ (delta)-receptors
Another special things opiods can do ? * can be agonists at one receptor AND antagonist at another
Receptor for Euphoria and Receptor for Dysphoria = ? * Mu = euphoris..... * Kappa = Dysphoria
Identify sites of opioid action in the ascending pain pathway = ? * Afferent Nociceptor, Dorsal Horn, and Ventral Caudal Thalamus
Systemic distribution of exogenous opioids does ? * causes the release of endogenous peptides.... * Overall effect is an INCREASE of analgesic effect (numbing the pain)
Opiod action on the Descending pain pathway = ? * Inhibits release of GABA, inhibiting pain neuron transmission.... * Sites: Periaqueductal gray, Rostral Ventral Medulla, and Dorsal Horn
Since opioids undergo an intense first-pass effect, the ____ Dose needs to be higher than the ____ Dose ? * ORAL.... * Parental..... * Exceptions (poor first pass): codeine and oxycodone
Main reservoir of drug = ? * Skeletal muscle
Metabolism of Morphine = ? * UGT makes Morphine-3 = inhibitory/GABA actions and can cause seizures, and makes Morphine-6 = longer analgesic affects
One Opiod that has NO active metabolite, and can ware off quickly = ? * Fentanyl
Turns Codeine in to Morphine = ? * CYP-2D6 -- can see ultra-rapid metabolizers (need less drug bc morphine is gets in to the system a lot faster) see more pronounced effect
CNS effects of opioids ? * Analgesia, Euphoria, Dysphoria, Sedation, Resp Depression (watch in COPD ppl), Cough Suppression, Miosis (pin prick pupils), Truncal rigidity (treat with NeuroMusc Blocker), Temp issues ( Mu agonists = hyperthermia, and Kappa agonists= hypo)
Peripheral effects of opioids = ? * bradycardia (except for meperidine = Tachy), slows down renal function, Uterus = prolongs labor, Neuroendocrine = ADH-prolactin, and Flushing/Warming Skin
Clinical use Example = ? * Used in CV and other high risk surgeries where goal is to minimize CV depression
**STRONG Agonist Drug List = ? ** * Morphine -- Hydromorphone -- Heroin -- Methadone -- Meperidine -- Fentanyl
**MILD/MOD Agonist Drug List = ? ** * Codeine -- Hydrocodone -- Oxycodone -- Loperamide -- Diphenoxylate
**MIXED Receptor Agonist = ? ** * Buprenorphine
**Antagonist Drug List = ? ** * Naloxone -- Naltrexone
**Miscellaneous Drug List = ? ** * Tramadol -- Dextromethorphan
Methadone uses = ? * To alleviate long term/chronic pain due to its long t 1/2.... * Withdrawal CxSx less likely too (can use for withdrawal pts too)
Fentanyl = ? * widely used and is safe since no active metabolite
Meperidine = ? * Has significant anti-muscarinic effects (anti-DUMBBELSS).... * Negative inotropic action on the heart (CI in Tachy).... * Can cause Seizures or renal failure
Codeine = ? * antitussive (cough).... * Watch monoamine oxidase inhibitor use with this drug.... * Consider a NO GO in kids due to metabolism
Hydrocodone and Oxycodone = ? * Less efficacious than morphine.... *Often combined with acetaminophen for mild to moderate pain..... * HYDROS = NOT used in Migraines
Diphenoxylate and Loperamide = ? * Used in the treatment of diarrhea.... * used with atropine (anti-musc) to stop abuse potential
Antagonists primarily through µ-opioid receptors = ? * Naloxone - IV and Naltrexone - Oral (Used for addicts in treatment programs and has use with alcoholics)
Patient has a an opioid overdose and alcohol overdose, what do you give them = ? * use Naltraxone....* Naloxone = use in OPIOD ONLY !
Naloxone SE = ? * A severely depressed (resp/CV) patient may recover for 1-2 hours then relapse – so monitor tmt
Buprenorphine = ? * SUBLINGUAL route.... * Potent and long-acting partial µ-receptor agonist and κ-receptor antagonist ..... * Use: analgesia and maintenance therapy during opioid withdrawal
Tramadol = ? * serotonin re-uptake blocker.... * is an adjunct.... * watch use in other serotonin re-uptake blockers bc = Serotonin Syndrome
Dextromethorphan = ? * Antitussive (cough)... * Kids Under 6 = BANNED
Contraindications/Cautions = ? * Pure agonists with weak partial agonists – risk of diminished analgesia or inducing a withdrawal state (bc partial gets there first).... * don't give if there is an increase in intracranial pressure .... * NO in Pregnants
Some things that we never develop tolerance too ? * Miosis (pin prick pupil) and Constipation
Tolerance is minimized by ? * giving smaller doses with longer intervals between dosing..... * tolerance is also usu to Mu-Rec... * also depends on the individual
Dependence/ Withdrawal CxSx of a PURE agonist = ? * yawning, mydriasis, anxiety, hostility
Mixed = ? * appetite and weight loss, abdominal cramps
Created by: thamrick800